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EP3286169A4 - Novel compounds - Google Patents

Novel compounds Download PDF

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Publication number
EP3286169A4
EP3286169A4 EP16783708.7A EP16783708A EP3286169A4 EP 3286169 A4 EP3286169 A4 EP 3286169A4 EP 16783708 A EP16783708 A EP 16783708A EP 3286169 A4 EP3286169 A4 EP 3286169A4
Authority
EP
European Patent Office
Prior art keywords
novel compounds
novel
compounds
Prior art date
Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
Granted
Application number
EP16783708.7A
Other languages
German (de)
French (fr)
Other versions
EP3286169A2 (en
EP3286169B1 (en
Inventor
Linda N. Casillas
John David Harling
Afjal Hussain MIAH
Mark David RACKHAM
Ian Edward David Smith
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
GlaxoSmithKline Intellectual Property Development Ltd
Original Assignee
GlaxoSmithKline Intellectual Property Development Ltd
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by GlaxoSmithKline Intellectual Property Development Ltd filed Critical GlaxoSmithKline Intellectual Property Development Ltd
Publication of EP3286169A2 publication Critical patent/EP3286169A2/en
Publication of EP3286169A4 publication Critical patent/EP3286169A4/en
Application granted granted Critical
Publication of EP3286169B1 publication Critical patent/EP3286169B1/en
Active legal-status Critical Current
Anticipated expiration legal-status Critical

Links

Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/47Quinolines; Isoquinolines
    • A61K31/472Non-condensed isoquinolines, e.g. papaverine
    • A61K31/4725Non-condensed isoquinolines, e.g. papaverine containing further heterocyclic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D403/00Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Rheumatology (AREA)
  • Pain & Pain Management (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Peptides Or Proteins (AREA)
EP16783708.7A 2015-04-22 2016-04-20 Protac compounds modulating rip2 kinase activity Active EP3286169B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB1506872.9A GB201506872D0 (en) 2015-04-22 2015-04-22 Novel compounds
PCT/US2016/028332 WO2016172134A2 (en) 2015-04-22 2016-04-20 Novel compounds

Publications (3)

Publication Number Publication Date
EP3286169A2 EP3286169A2 (en) 2018-02-28
EP3286169A4 true EP3286169A4 (en) 2018-11-21
EP3286169B1 EP3286169B1 (en) 2020-10-07

Family

ID=53299021

Family Applications (1)

Application Number Title Priority Date Filing Date
EP16783708.7A Active EP3286169B1 (en) 2015-04-22 2016-04-20 Protac compounds modulating rip2 kinase activity

Country Status (21)

Country Link
US (2) US10435391B2 (en)
EP (1) EP3286169B1 (en)
JP (1) JP2018513867A (en)
KR (1) KR20170139096A (en)
CN (1) CN107709305B (en)
AU (1) AU2016252404B2 (en)
BR (1) BR112017022604A2 (en)
CA (1) CA2983414A1 (en)
CL (1) CL2017002650A1 (en)
CO (1) CO2017011851A2 (en)
CR (1) CR20170478A (en)
EA (1) EA033343B1 (en)
ES (1) ES2841548T3 (en)
GB (1) GB201506872D0 (en)
HK (1) HK1243410A1 (en)
IL (1) IL255067A0 (en)
MX (1) MX375674B (en)
PE (1) PE20180044A1 (en)
PH (1) PH12017501921A1 (en)
SG (1) SG11201708311UA (en)
WO (1) WO2016172134A2 (en)

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US10071164B2 (en) * 2014-08-11 2018-09-11 Yale University Estrogen-related receptor alpha based protac compounds and associated methods of use
US12312316B2 (en) 2015-01-20 2025-05-27 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
US11352351B2 (en) 2015-01-20 2022-06-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
HK1249058A1 (en) 2015-03-18 2018-10-26 Arvinas, Inc. Compounds and methods for the enhanced degradation of targeted proteins
GB201506872D0 (en) 2015-04-22 2015-06-03 Ge Oil & Gas Uk Ltd Novel compounds
WO2016197114A1 (en) 2015-06-05 2016-12-08 Arvinas, Inc. Tank-binding kinase-1 protacs and associated methods of use
US10772962B2 (en) 2015-08-19 2020-09-15 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of bromodomain-containing proteins
CA3020792A1 (en) * 2016-04-20 2017-10-26 Glaxosmithkline Intellectual Property Development Limited Conjugates comprising ripk2 inhibitors
WO2018053354A1 (en) 2016-09-15 2018-03-22 Arvinas, Inc. Indole derivatives as estrogen receptor degraders
HUE070289T2 (en) 2016-10-11 2025-05-28 Arvinas Operations Inc Compounds and methods for the targeted degradation of androgen receptor
KR20230127371A (en) 2016-11-01 2023-08-31 아비나스 오퍼레이션스, 인코포레이티드 Tau-protein targeting protacs and associated methods of use
IL297717A (en) 2016-12-01 2022-12-01 Arvinas Operations Inc Tetrahydronaphthalene and tetrahydroisoquinoline derivatives as estrogen receptor degraders
WO2018118598A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Compounds and methods for the targeted degradation of fetal liver kinase polypeptides
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WO2018119441A1 (en) 2016-12-23 2018-06-28 Arvinas, Inc. Egfr proteolysis targeting chimeric molecules and associated methods of use
US11173211B2 (en) 2016-12-23 2021-11-16 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of rapidly accelerated Fibrosarcoma polypeptides
US11191741B2 (en) 2016-12-24 2021-12-07 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of enhancer of zeste homolog 2 polypeptide
IL300417A (en) 2017-01-26 2023-04-01 Arvinas Operations Inc Bifunctional benzthiophene compounds, compositions comprisng them and their use in treatment
EP3577109A4 (en) 2017-01-31 2020-11-18 Arvinas Operations, Inc. CEREBLON LIGANDS AND BIFUNCTIONAL CONNECTIONS THEREOF
US11065231B2 (en) 2017-11-17 2021-07-20 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of interleukin-1 receptor- associated kinase 4 polypeptides
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EP3743066A4 (en) 2018-01-26 2021-09-08 Yale University IMIDE BASED MODULATORS OF PROTEOLYSIS AND METHOD OF USE
JP7720698B2 (en) 2018-04-04 2025-08-08 アルビナス・オペレーションズ・インコーポレイテッド Modulators of protein degradation and related methods of use
EP3831811A4 (en) 2018-07-31 2022-04-20 Fimecs, Inc. Heterocyclic compound
CN112912376A (en) 2018-08-20 2021-06-04 阿尔维纳斯运营股份有限公司 Proteolytic targeted chimeric (PROTAC) compounds with E3 ubiquitin ligase binding activity and targeting alpha-synuclein for the treatment of neurodegenerative diseases
WO2020043122A1 (en) * 2018-08-28 2020-03-05 南京明德新药研发有限公司 Quinazoline derivatives as rip2 kinase inhibitor
US11547759B2 (en) 2019-01-30 2023-01-10 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US11098025B2 (en) 2019-01-30 2021-08-24 Montelino Therapeutics, Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US12233356B2 (en) 2019-03-21 2025-02-25 Lonza Sales Ag Process for preparing extracellular vesicles
US20240108747A1 (en) 2019-03-21 2024-04-04 Lonza Sales Ag Extracellular vesicle conjugates and uses thereof
US11912699B2 (en) 2019-07-17 2024-02-27 Arvinas Operations, Inc. Tau-protein targeting compounds and associated
JP2021024787A (en) 2019-07-31 2021-02-22 ファイメクス株式会社 Heterocyclic compound
JP7764027B2 (en) 2019-07-31 2025-11-05 ファイメクス株式会社 heterocyclic compounds
EP4021450B1 (en) 2019-08-26 2025-11-05 Arvinas Operations, Inc. Methods of treating breast cancer with tetrahydronaphthalene derivatives as estrogen receptor degraders
AU2020368542B2 (en) 2019-10-17 2024-02-29 Arvinas Operations, Inc. Bifunctional molecules containing an E3 ubiquitine ligase binding moiety linked to a BCL6 targeting moiety
AU2020405129A1 (en) 2019-12-19 2022-06-23 Arvinas Operations, Inc. Compounds and methods for the targeted degradation of androgen receptor
MX2022014071A (en) 2020-05-09 2023-01-30 Arvinas Operations Inc Methods of manufacturing a bifunctional compound, ultrapure forms of the bifunctional compound, and dosage forms comprising the same.
WO2021237100A1 (en) 2020-05-21 2021-11-25 Codiak Biosciences, Inc. Methods of targeting extracellular vesicles to lung
EP4204418A1 (en) 2020-08-28 2023-07-05 Arvinas Operations, Inc. Rapidly accelerating fibrosarcoma protein degrading compounds and associated methods of use
EP4211128A1 (en) 2020-09-14 2023-07-19 Arvinas Operations, Inc. Crystalline forms of a compound for the targeted degradation of estrogen receptor
WO2022061348A1 (en) * 2020-09-16 2022-03-24 Biotheryx, Inc. Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
WO2022066928A2 (en) 2020-09-23 2022-03-31 Codiak Biosciences, Inc. Process for preparing extracellular vesicles
WO2022197862A1 (en) * 2021-03-17 2022-09-22 Biotheryx, Inc. Sos1 protein degraders, pharmaceutical compositions thereof, and their therapeutic applications
EP4323352A1 (en) 2021-04-16 2024-02-21 Arvinas Operations, Inc. Modulators of bcl6 proteolysis and associated methods of use
US11981672B2 (en) 2021-09-13 2024-05-14 Montelino Therapeutics Inc. Bi-functional compounds and methods for targeted ubiquitination of androgen receptor
US12419962B2 (en) 2022-03-16 2025-09-23 Biotheryx, Inc. Quinazolines, pharmaceutical compositions, and therapeutic applications
EP4499628A1 (en) 2022-03-24 2025-02-05 GlaxoSmithKline Intellectual Property Development Limited 2,4-dioxotetrahydropyrimidinyl derivatives as degrons in protacs
TW202432544A (en) 2022-09-07 2024-08-16 美商亞文納營運公司 Rapidly accelerated fibrosarcoma (raf) degrading compounds and associated methods of use
CN115869308B (en) * 2022-12-30 2024-03-26 中山大学肿瘤防治中心(中山大学附属肿瘤医院、中山大学肿瘤研究所) Application of a small molecule compound in the preparation of anti-colorectal cancer drugs
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Also Published As

Publication number Publication date
JP2018513867A (en) 2018-05-31
WO2016172134A2 (en) 2016-10-27
US20190382381A1 (en) 2019-12-19
SG11201708311UA (en) 2017-11-29
PE20180044A1 (en) 2018-01-15
US20180134688A1 (en) 2018-05-17
BR112017022604A2 (en) 2018-07-17
EA033343B1 (en) 2019-09-30
ES2841548T3 (en) 2021-07-08
EP3286169A2 (en) 2018-02-28
AU2016252404B2 (en) 2018-07-26
CR20170478A (en) 2018-01-22
CO2017011851A2 (en) 2018-02-09
GB201506872D0 (en) 2015-06-03
HK1243410A1 (en) 2018-07-13
MX2017013556A (en) 2018-08-01
PH12017501921A1 (en) 2018-03-19
CL2017002650A1 (en) 2018-03-16
AU2016252404A1 (en) 2017-12-07
US10435391B2 (en) 2019-10-08
EP3286169B1 (en) 2020-10-07
CN107709305B (en) 2020-09-29
WO2016172134A3 (en) 2016-12-01
KR20170139096A (en) 2017-12-18
CN107709305A (en) 2018-02-16
MX375674B (en) 2025-03-06
CA2983414A1 (en) 2016-10-27
EA201792047A1 (en) 2018-04-30
IL255067A0 (en) 2017-12-31

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